摘要
目的: 研究盐酸小檗碱(BBR)与地高辛(DIG)合用对大鼠体内DIG药动学的影响。 方法: 大鼠随机分为DIG单用组和DIG+BBR低、中、高剂量合用组。大鼠单剂量或多剂量给予BBR后,放免法测定单次口服DIG的血药浓度。药-时数据经3P97药动学软件处理,获得各组药动学参数。 结果: 合用后,BBR在低剂量时(10 mg·kg-1)对DIG的药动学过程无显著影响;但在中、高剂量(30,100 mg·kg-1)时有显著影响,AUC0~t分别增加了33%,70%(单剂量)和27%,75%(多剂量)(P〈0.05)。 结论: 体内研究表明BBR与DIG合用时,在一定浓度范围内,可明显提高其生物利用度,其机制可能与BBR抑制肠道P-糖蛋白有关。
Objective : To study the effects of berberine (BBR) on the pharmacokinetics of digoxin (DIG) in rats. Method: Rats were randomly assigned into DIG, low dose-BBR, middle dose-BBR and high dose-BBR group. After singe or a 2-week ig pretreatment with BBR, serum DIG concentration was determined by radioimmunoassay. Pharmacokinetic calculations were performed on each individual set of data using 3P97 practical pharmacokinetic software. Result: No significant difference was found between the control and 10 mg·kg-1BBR combined group. After pretreatment with BBR (30,100 mg·kg-1), the pharmacokinetic parameters of ig DIG were significantly altered. The AUC0~t of DIG with BBR increased by 33% and 70%(single), 27% and 75% (2-week), respectively. Conclusion: BBR increases bioavailability of DIG, which may be related to its inhibition effect on intestinal P-gp.
出处
《中国中药杂志》
CAS
CSCD
北大核心
2011年第7期918-921,共4页
China Journal of Chinese Materia Medica